登録情報 | データベース: PDB / ID: 8aqn |
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タイトル | Crystal structure of PPARG and NCOR2 with BAY-4931, an inverse agonist (compound 6c) |
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要素 | - Nuclear receptor corepressor 2
- Peroxisome proliferator-activated receptor gamma
PPARγ |
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キーワード | TRANSCRIPTION (転写 (生物学)) / nuclear hormone receptor transcription factor |
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機能・相同性 | 機能・相同性情報
Loss of MECP2 binding ability to the NCoR/SMRT complex / negative regulation of androgen receptor signaling pathway / regulation of cellular ketone metabolic process / nuclear glucocorticoid receptor binding / prostaglandin receptor activity / regulation of cholesterol transporter activity / negative regulation of connective tissue replacement involved in inflammatory response wound healing / negative regulation of receptor signaling pathway via STAT / MECP2 regulates transcription factors / negative regulation of extracellular matrix assembly ...Loss of MECP2 binding ability to the NCoR/SMRT complex / negative regulation of androgen receptor signaling pathway / regulation of cellular ketone metabolic process / nuclear glucocorticoid receptor binding / prostaglandin receptor activity / regulation of cholesterol transporter activity / negative regulation of connective tissue replacement involved in inflammatory response wound healing / negative regulation of receptor signaling pathway via STAT / MECP2 regulates transcription factors / negative regulation of extracellular matrix assembly / Notch binding / negative regulation of vascular endothelial cell proliferation / negative regulation of cellular response to transforming growth factor beta stimulus / negative regulation of cardiac muscle hypertrophy in response to stress / arachidonic acid binding / positive regulation of low-density lipoprotein receptor activity / positive regulation of adiponectin secretion / lipoprotein transport / negative regulation of sequestering of triglyceride / macrophage derived foam cell differentiation / positive regulation of vascular associated smooth muscle cell apoptotic process / DNA binding domain binding / STAT family protein binding / positive regulation of fatty acid metabolic process / response to lipid / NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis / negative regulation of SMAD protein signal transduction / Notch-HLH transcription pathway / LBD domain binding / negative regulation of type II interferon-mediated signaling pathway / negative regulation of cholesterol storage / E-box binding / alpha-actinin binding / lipid homeostasis / negative regulation of vascular associated smooth muscle cell proliferation / R-SMAD binding / monocyte differentiation / negative regulation of macrophage derived foam cell differentiation / cellular response to low-density lipoprotein particle stimulus / negative regulation of lipid storage / negative regulation of blood vessel endothelial cell migration / Regulation of MECP2 expression and activity / negative regulation of BMP signaling pathway / white fat cell differentiation / negative regulation of mitochondrial fission / estrous cycle / positive regulation of cholesterol efflux / retinoic acid receptor signaling pathway / positive regulation of fat cell differentiation / negative regulation of osteoblast differentiation / 細胞分化 / positive regulation of DNA binding / BMP signaling pathway / long-chain fatty acid transport / nuclear retinoid X receptor binding / negative regulation of signaling receptor activity / regulation of cellular response to insulin stimulus / cell maturation / NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux / response to organonitrogen compound / epithelial cell differentiation / positive regulation of adipose tissue development / peroxisome proliferator activated receptor signaling pathway / 授乳 / transcription repressor complex / Regulation of lipid metabolism by PPARalpha / hormone-mediated signaling pathway / negative regulation of angiogenesis / cerebellum development / response to nutrient / SUMOylation of transcription cofactors / negative regulation of miRNA transcription / negative regulation of MAP kinase activity / fatty acid metabolic process / Regulation of PTEN gene transcription / HDACs deacetylate histones / transcription coregulator binding / placenta development / Downregulation of SMAD2/3:SMAD4 transcriptional activity / negative regulation of smooth muscle cell proliferation / peptide binding / negative regulation of transforming growth factor beta receptor signaling pathway / SUMOylation of intracellular receptors / mRNA transcription by RNA polymerase II / regulation of circadian rhythm / lipid metabolic process / PPARA activates gene expression / Cytoprotection by HMOX1 / NOTCH1 Intracellular Domain Regulates Transcription / Constitutive Signaling by NOTCH1 PEST Domain Mutants / Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants / 血圧 / DNA-binding transcription repressor activity, RNA polymerase II-specific / positive regulation of DNA-binding transcription factor activity / nuclear matrix / histone deacetylase binding / negative regulation of inflammatory response / positive regulation of miRNA transcription / Transcriptional regulation of white adipocyte differentiation / HCMV Early Events類似検索 - 分子機能 N-CoR, GPS2-interacting domain / G-protein pathway suppressor 2-interacting domain / SANT domain profile. / SANT domain / PPARγ / Peroxisome proliferator-activated receptor gamma, N-terminal / PPAR gamma N-terminal region / Myb domain / Myb-like DNA-binding domain / PPAR ... N-CoR, GPS2-interacting domain / G-protein pathway suppressor 2-interacting domain / SANT domain profile. / SANT domain / PPARγ / Peroxisome proliferator-activated receptor gamma, N-terminal / PPAR gamma N-terminal region / Myb domain / Myb-like DNA-binding domain / PPAR / SANT SWI3, ADA2, N-CoR and TFIIIB'' DNA-binding domains / SANT/Myb domain / Homeobox-like domain superfamily / 核内受容体 / Nuclear hormones receptors DNA-binding region signature. / Zinc finger, nuclear hormone receptor-type / Zinc finger, C4 type (two domains) / Nuclear hormone receptors DNA-binding domain profile. / c4 zinc finger in nuclear hormone receptors / Nuclear hormone receptor, ligand-binding domain / Nuclear hormone receptor-like domain superfamily / Ligand-binding domain of nuclear hormone receptor / Nuclear receptor (NR) ligand-binding (LBD) domain profile. / Ligand binding domain of hormone receptors / Zinc finger, NHR/GATA-type類似検索 - ドメイン・相同性Chem-O0U / PPARγ / Nuclear receptor corepressor 2類似検索 - 構成要素 |
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生物種 | ![](img/tx_human.gif) Homo sapiens (ヒト) |
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手法 | X線回折 / シンクロトロン / 分子置換 / 解像度: 1.9 Å |
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データ登録者 | Friberg, A. / Orsi, D.L. / Pook, E. / Braeuer, N. / Lemke, C.T. / Stellfeld, T. / Puetter, V. / Goldstein, J. |
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資金援助 | 1件 |
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引用 | ジャーナル: J.Med.Chem. / 年: 2022 タイトル: Discovery and Structure-Based Design of Potent Covalent PPAR gamma Inverse-Agonists BAY-4931 and BAY-0069 . 著者: Orsi, D.L. / Pook, E. / Brauer, N. / Friberg, A. / Lienau, P. / Lemke, C.T. / Stellfeld, T. / Bruggemeier, U. / Putter, V. / Meyer, H. / Baco, M. / Tang, S. / Cherniack, A.D. / Westlake, L. / ...著者: Orsi, D.L. / Pook, E. / Brauer, N. / Friberg, A. / Lienau, P. / Lemke, C.T. / Stellfeld, T. / Bruggemeier, U. / Putter, V. / Meyer, H. / Baco, M. / Tang, S. / Cherniack, A.D. / Westlake, L. / Bender, S.A. / Kocak, M. / Strathdee, C.A. / Meyerson, M. / Eis, K. / Goldstein, J.T. |
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履歴 | 登録 | 2022年8月12日 | 登録サイト: PDBE / 処理サイト: PDBE |
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改定 1.0 | 2022年11月9日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2022年11月23日 | Group: Database references / カテゴリ: citation / citation_author Item: _citation.journal_volume / _citation.page_first ..._citation.journal_volume / _citation.page_first / _citation.page_last / _citation.title / _citation_author.identifier_ORCID |
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改定 1.2 | 2022年12月28日 | Group: Structure summary / カテゴリ: struct / Item: _struct.title |
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改定 1.3 | 2024年5月1日 | Group: Data collection / Refinement description カテゴリ: chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model |
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